28th week of 2012 patent applcation highlights part 45 |
Patent application number | Title | Published |
20120178679 | FUSED AROMATIC PTP-IB INHIBITORS - The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes. | 2012-07-12 |
20120178680 | GLYCOSIDE DERIVATIVES AND USES THEREOF - This invention relates to compounds represented by formula (I): | 2012-07-12 |
20120178681 | BIPIPERIDINYL COMPOUNDS, COMPOSITIONS, CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. | 2012-07-12 |
20120178682 | GB1 Peptidic Compounds and Methods for Making and Using the Same - GB1 peptidic compounds that specifically bind to a target molecule are provided. Also provided are methods for making and using the compounds. These compounds and methods find use in a variety of applications in which specific binding to target molecules, e.g., target proteins, is desired. | 2012-07-12 |
20120178683 | VEGF ANTAGONIST FORMULATIONS - Formulations of a vascular endothelial growth factor (VEGF)-specific fusion protein antagonist are provided including a pre-lyophilized formulation, a reconstituted lyophilized formulation, and a stable liquid formulation. Preferably, the fusion protein has the sequence of SEQ ID NO:4. | 2012-07-12 |
20120178684 | Surgical Calcium Phosphate Citrate-Containing Cement and Method of Manufacturing the Same - The present invention discloses a surgical cement and a manufacturing method thereof. The surgical cement comprises a cementing component selected form the group of a basic calcium phosphate consisting of tetracalcium phosphate, alpha-tricalcium phosphate, decomposed hydroxyapatite, or a combination thereof; a setting reagent selected form the group of an acidic calcium citrate consisting of monocalcium citrate, dicalcium citrate, or a combination thereof; and water; wherein a weight ratio of the cementing component and the setting reagent ranges from about 1:1 to about 8:1. The surgical cement is bioresorbable and bioactive and is useful in orthopedic, maxillofacial and dental applications. In addition, the surgical cement of this invention has a good flow character and a relatively short setting time. | 2012-07-12 |
20120178685 | FGF21 MUTANTS AND USES THEREOF - The invention provides nucleic acid molecules encoding FGF21 mutant polypeptides, FGF21 mutant polypeptides, pharmaceutical compositions comprising FGF21 mutant polypeptides, and methods for treating metabolic disorders using such nucleic acids, polypeptides, or pharmaceutical compositions. | 2012-07-12 |
20120178686 | CHEMICAL INDUCTION OF LACTATION - The present invention describes a method of inducing lactation in non-human mammals by using a single administrations of an estrogen compound, a dopaminergic antagonist, and oxytocin. For example, the estrogen compound may be a long acting composition and is administered at least one week before the dopaminergic antagonist. However, the oxytocin administration may be given the day after the dopaminergic antagonist, after which lactation may begin immediately. Preferred compounds may comprise a non-17β estradiol and domperidone. Such an injection protocol has resulted in the production of commercially viable volumes of milk from transgenic pigs. | 2012-07-12 |
20120178687 | Suspension formulations of insulinotropic peptides and uses thereof - A suspension formulation of an insulinotropic peptide (e.g., glucagon-like peptide-1 (GLP-1) or exenatide) is described. The suspension formulation comprises (i) a non-aqueous, single-phase vehicle, comprising one or more polymer and one or more one solvent, wherein the vehicle exhibits viscous fluid characteristics, and (ii) a particle formulation comprising the insulinotropic peptide, wherein the peptide is dispersed in the vehicle. The particle formulation further includes a stabilizing component comprising one or more stabilizers, for example, carbohydrates, antioxidants, amino acids, and buffers. Devices for delivering the suspension formulations and methods of use are also described. | 2012-07-12 |
20120178688 | THERAPEUTIC AGENTS FOR REDUCING PARATHYROID HORMONE LEVELS - Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X | 2012-07-12 |
20120178689 | METHODS OF TREATMENT WITH NATRIURETIC PEPTIDES - Methods of treating heart failure, or decreasing blood pressure, comprising administering an NP at an appropriate dose, or in an amount sufficient to provide particular concentrations of NP, are provided. | 2012-07-12 |
20120178690 | NOVEL NETRIN DERIVATIVES AND USES THEREOF - Netrin proteins and their receptors regulate cell and axon migration, and are implicated in tissue morphogenesis, tumorigenesis and angiogenesis. Deregulation of mechanisms that control cell motility plays a key role in tumor progression by promoting tumor cell dissemination. Unwanted neovascularization also contributes to tumor progression and metastasis and to ocular diseases which are a leading cause of blindness. Here, we describe novel netrin-derived polypeptides and fragments or derivatives thereof that selectively inhibit cell growth, migration or branching. Methods and compositions for the treatment and prevention of conditions involving cell migration or neovascularization, such as cancer and ocular disease, are also provided. | 2012-07-12 |
20120178691 | FACTOR VIII COMPOSITIONS AND METHODS OF MAKING AND USING SAME - The present invention relates to compositions comprising factor VIII coagulation factors linked to extended recombinant polypeptide (XTEN), isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of making and using such compositions in treatment of factor VIII-related diseases, disorders, and conditions. | 2012-07-12 |
20120178692 | DOSAGE FORMS OF POLYMER-FACTOR VIII MOIETY CONJUGATES - Conjugates of a Factor VIII moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided are compositions comprising the conjugates, methods of making the conjugates, and methods of administering compositions comprising the conjugates to a patient. | 2012-07-12 |
20120178693 | Cofactors for Thrombin Activation of Factor VII and Uses Thereof - The invention relates to fusion proteins that bind the enzyme thrombin and enhance the activation of the substrate Factor VII to the product Factor VIIa. The invention is also directed to polynucleotides, vectors, host cells, pharmaceutical compositions, and methods of treatment. | 2012-07-12 |
20120178694 | Modified Compstatin With Peptide Backbone And C-Terminal Modifications - Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. The compounds comprise compstatin analogs having a constrained backbone at position 8 (glycine) and, optionally, specific substitutions for threonine at position 13. | 2012-07-12 |
20120178695 | METHODS OF TREATING NEUROPATHIC PAIN - The disclosure relates, at least in part, to methods of treating neuropathic pain in a patient in need thereof by administering an effective amount of a disclosed compound, e.g. a peptide NMDA receptor partial agonist. | 2012-07-12 |
20120178696 | Compositions and Methods for Modulating AMPA Receptor-mediated Excitotoxicity - The present invention provides AMPAR excitotoxicity mediating polypeptides comprising the GluR2 NT1-3-2 (Y142-K172) amino acid sequence (SEQ ID NO:1) or the GAPDH(2-2-1-1) (I221-E250)amino acid sequence (SEQ ID NO:2). Also disclosed are nucleotide sequences encoding the polypeptides, methods of inhibiting GAPDH association with the GluR2 subunit or p53. Methods of inhibiting AMPA receptor mediated excitotoxicity using the polypeptides and nucleic acids are also disclosed. | 2012-07-12 |
20120178697 | Compositions and methods for the inhibition of dishevelled proteins - The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction. | 2012-07-12 |
20120178698 | Agents and Uses Thereof - The present invention provides agents capable of activating Sox11 for use in medicine. In particular, the agents of the invention are useful in the treatment of cancers, such as lymphomas (e.g. mantel cell lymphoma). The invention further provides pharmaceutical compositions of the agents of the invention, as well as methods and uses of the same. | 2012-07-12 |
20120178699 | KLOTHO PROTEIN AND RELATED COMPOUNDS FOR THE TREATMENT AND DIAGNOSIS OF CANCER - Disclosed is the use of a klotho protein or related compounds (especially KL1 or KL1 analogue) for treatment, and especially treatment of cancer, alone or together with other active pharmaceutical ingredients such as chemotherapeutic agents. | 2012-07-12 |
20120178700 | PEPTIDOMIMETIC MACROCYCLES - The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. | 2012-07-12 |
20120178701 | Melanocortin Receptor-Specific Peptides - Melanocortin receptor-specific cyclic peptides of the formula | 2012-07-12 |
20120178702 | STABLE LIPID-COMPRISING DRUG DELIVERY COMPLEXES AND METHODS FOR THEIR PRODUCTION - Novel stable, concentrated, biologically active and ready-to-use lipid-comprising drug delivery complexes and methods for their production are described. The biological activity of the complexes produced are comparable to the formulations prepared according to the prior art admixture method and upon purification, the complexes produced by the method of this invention are 50 to 500 fold more concentrated than the complexes formed by admixture. The method described herein provides for the large scale production of lipid-comprising drug delivery systems useful for gene therapy and other applications. | 2012-07-12 |
20120178703 | MULTIMERIC POLYPEPTIDES OF HLA-G INCLUDING AT LEAST TWO ALPHA3 DOMAINS AND PHARMACEUTICAL USES THEREOF - Multimeric polypeptides and pharmaceutical uses thereof; multimers comprising alpha3 peptides of an HLA-G antigen and methods of producing such multimers, pharmaceutical compositions comprising the same, as well as their uses for treating various diseases including organ/tissue rejection. | 2012-07-12 |
20120178704 | PREVENTION AND TREATMENT OF COLON CANCER - Stilbene compounds for the prevention and treatment of colon cancer or colon inflammation and methods of using same are provided. | 2012-07-12 |
20120178705 | METHODS FOR PREPARATION OF GLYCOSPHINGOLIPIDS AND USES THEREOF - Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of α-galactosyl ceramide, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells. | 2012-07-12 |
20120178706 | METHOD FOR PREPARING A CENTELLA ASIATICA EXTRACT RICH IN MADECASSOSIDE AND IN TERMINOLOSIDE - The invention concerns an extract of | 2012-07-12 |
20120178707 | METHODS FOR TREATING PROSTRATE CONDITIONS - Methods for treating prostate cancer involving the administration of a compound that selectively inhibits pathological production of human vascular endothelial growth factor (VEGF) are described. Methods for treating benign prostatic hyperplasia involving the administration of a compound that selectively inhibits pathological production of human VEGF are also described. The compound may be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment. | 2012-07-12 |
20120178708 | PHENETHYLSULFONE ISOINDOLINE DERIVATIVES AND THEIR USE - Provided are phenethyl isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed. | 2012-07-12 |
20120178709 | CRYSTALLINE PHASES OF 5,6-DFICHLORO-2-(ISOPROPYLAMINO)-1- -L-RIBOFURANOSYL)-1H-BENZIMIDAZOLE - The invention relates to novel crystalline phases of 5,6-dichloro-2-(isopropylamino)-1-(β-L-ribofuranosyl)-1H-benzimidazole (Maribavir), pharmaceutical compositions thereof and their use in medical therapy. | 2012-07-12 |
20120178710 | SYNTHESIS OF CYCLIC DIGUANOSINE MONOPHOSPHATE AND THIOPHOSPHATE ANALOGS THEREOF - The invention provides methods for the synthesis of cyclic dinucleotides and thiophosphate analogs thereof as well as a new family of analogs of cyclic diguanosine monophosphate that includes a series of seven phosphorothioate derivatives that includes diastereomers of mono-, di-, and trithiophosphates. | 2012-07-12 |
20120178711 | CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTICS DELIVERY - The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein. | 2012-07-12 |
20120178712 | PHYTOCHEMICAL COMPOSITIONS INCLUDING SESAMIN FOR ANTI-INFLAMMATORY, ANTI-CYTOKINE STORM, AND OTHER USES - A composition (e.g., phytochemical composition) including sesamin, the composition exhibiting anti-inflammatory, anti-cytokine storm, connective tissue preservation, anti-viral, and/or other properties in biological tissue. The phytochemical composition therapeutically affects a pro-inflammatory cytokine condition, for instance facilitating or effectuating decrease in a quantity of a pro-inflammatory cytokine, for example, interleukin-1 and tumor necrosis-alpha. The phytochemical composition facilitates or effectuates an increase in quantity of an anti-inflammatory cytokines. The phytochemical composition can additionally facilitate a connective tissue extracellular matrix (ECM) preservation effect. The phytochemical composition can also inhibit an action of a viral neuraminidase, for example, the influenza A virus neuraminidase. Uses of sesamin for the manufacture of phytochemical compositions having predetermined concentrations of sesamin include one or more of facilitating a decrease in quantity of pro-inflammatory cytokines, an increase in anti-inflammatory cytokines, a connective tissue anti-degenerative effect, and/or an inhibition of viral neuraminidase within the living organism. Manufacturing processes for the phytochemical compositions are also described. | 2012-07-12 |
20120178713 | PHENYL SULPHONAMIDES AS MODULATORS OF ION CHANNELS - The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain. | 2012-07-12 |
20120178714 | Phosphorus-containing Compounds & Uses Thereof - This disclosure concerns a new family of phosphorus-containing compounds of Formula (I): | 2012-07-12 |
20120178715 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS - Compounds of Formula I: and salts thereof in which R | 2012-07-12 |
20120178716 | Unsaturated Heterocyclic Derivatives - This invention relates to compounds of the general formula: | 2012-07-12 |
20120178717 | 4-QUINOLINEMETHANOLS AS ANTI-MALARIAL AGENTS - The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases. | 2012-07-12 |
20120178718 | NOVEL IMIDAZOLIDINE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS - Novel compounds are disclosed that have a Formula represented by the following: | 2012-07-12 |
20120178719 | MODULATION OF PHOSPHOLIPASE D FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - The present invention relates to methods of treating neurodegenerative diseases comprising administering, to a subject in need of such treatment, one or more agent that inhibits or reduces the action, including the catalytic activity, of an enzyme of the phospholipase D family, such as phospholipase D1 and/or phospholipase D2. The present invention also relates to cell-based assays which may be used to identify agents that inhibit or reduce the activity of enzymes of the phospholipase D family and that may be used in the treatment of neurodegenerative diseases. | 2012-07-12 |
20120178720 | Bisphosphonates as Inhibitors of Acid Sphingomyelinase - The present invention refers to bisphosphonate and phosphonate/phosphate compounds of Formulae I and its use as inhibitors of aSMase enzyme activity. | 2012-07-12 |
20120178721 | IMMUNOMODULATORY COMPOUNDS AND TREATMENT OF DISEASES RELATED TO AN OVERPRODUCTION OF INFLAMMATORY CYTOKINES - Method of using immunomodulatory compounds for treating diseases related to an overproduction of inflammatory cytokines, including diseases selected from asthma, atopic dermatitis, allergic rhinitis, prostatitis, inflammatory bowel disease, diabetes, and rheumatoid arthritis, the compounds being of general formula (I): | 2012-07-12 |
20120178722 | SYNERGISTIC ANTIMICROBIAL COMPOSITION - A synergistic antimicrobial composition having two components. The first component is a hydroxymethyl-substituted phosphorus compound. The second component is cis-1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane chloride. | 2012-07-12 |
20120178723 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IA-a or IB-a and subsets thereof: | 2012-07-12 |
20120178724 | Compositions for Reducing the Incidence of Drug Induced Arrhythmia - In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg. | 2012-07-12 |
20120178725 | METHOD OF MODULATING SHIP ACTIVITY - A method of treating or preventing an immune disorder, such as graft versus host disease, in a subject. The method includes the administering a SHIP1 inhibitor, such as 3α-aminocholestane, to a subject in need of treatment. Thus, SHIP1 inhibitors taught herein represent a novel class of small molecules that have the potential to enhance allogeneic transplantation, boost innate immunity and improve the treatment of hematologic malignancies. | 2012-07-12 |
20120178726 | NOVEL COMPOUNDS - The present invention provides compounds of formula (I) | 2012-07-12 |
20120178727 | COMBINATION AND COMPOSITION THAT CONTAINS AN ANTIMICROBIAL, A GLUCOCORTICOID AND AN ANTIMYCOTIC - The present invention relates to a topical pharmaceutical composition that comprises the combination of an antimicrobial, a glucocorticoid, an antimycotic and pharmaceutically acceptable vehicles or excipients; the method for producing the composition and the use of said composition for treating localized dermatosis ailments. | 2012-07-12 |
20120178728 | USE OF A COPOLYMER IN THE FORM OF A SOLUBILISER FOR A POORLY WATER-SOLUBLE COMPOUND - The use of copolymers obtained by free-radical polymerization of a mixture of
| 2012-07-12 |
20120178729 | CRYSTALLINE FORM I ROSUVASTATIN ZINC SALT - The present invention relates to crystalline Form I rosuvastatin zinc (2:1) salt, method of preparation thereof and use thereof as pharmaceutically active ingredient for the treatment of diseases related to lipid metabolism including hyperlipoproteinemia, hypercholesteremia, dyslipidemia and atherosclerosis. | 2012-07-12 |
20120178730 | SOD-IMITATING METAL COMPLEXES - The present invention comprises a process to synthesise metal complexes from macrocyclic polyazapyridinophane compounds characterised as superoxide dismutase enzyme (SOD) mimetics. Furthermore, the present invention relates to the macrocyclic polyazapyridinophane compounds themselves, the metal complexes formed from these and to their use in the treatment of diseases the aetiology of which is based on disturbances in the activity of, or a deficiency in endogenous SOD, mainly as anti-inflammatories, analgesics and antioxidant compounds providing protection against cellular oxidative stress. | 2012-07-12 |
20120178731 | NASAL, WOUND AND SKIN FORMULATIONS AND METHODS FOR CONTROL OF ANTIBIOTIC-RESISTANT STAPHYLOCOCCI AND OTHER GRAM-POSITIVE BACTERIA - Formulations and methods are disclosed which are effective to kill or control bacteria in the nares including gram-positive bacteria strains of | 2012-07-12 |
20120178732 | Biphenyloxyacetic Acid Derivatives for the Treatment of Respiratory Disease - The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim | 2012-07-12 |
20120178733 | FACTOR XA INHIBITORS - The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 2012-07-12 |
20120178734 | DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES - Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. | 2012-07-12 |
20120178735 | 2H-CHROMENE COMPOUND AND DERIVATIVE THEREOF - Provided is a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action. The 2H-chromene compound or derivative is particularly useful for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. | 2012-07-12 |
20120178736 | BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE - Formula I (Ia and Ib) compounds wherein (i) X | 2012-07-12 |
20120178737 | Tricyclic Heterocyclic Compounds as Phosphoinositide 3-Kinase Inhibitors - Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C | 2012-07-12 |
20120178738 | DIBENZO [B,F] [1,4]OXAZAPINE COMPOUNDS - The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4]oxazapine compounds of the formula: | 2012-07-12 |
20120178739 | LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 2012-07-12 |
20120178740 | HETEROCYCLIC COMPOUNDS AS JAK RECEPTOR AND PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to compounds of general formula (I) wherein A, R | 2012-07-12 |
20120178741 | Sulfonylamino-Derivatives As Novel Inhibitors Of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 2012-07-12 |
20120178742 | METABOTROPIC GLUTAMATE RECEPTOR MODULATORS - The invention relates to heterocyclic derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders. | 2012-07-12 |
20120178743 | NOVEL ADENINE COMPOUND AND USE THEREOF - An antiallergic agent for topical administration containing an adenine compound of general formula (1): | 2012-07-12 |
20120178744 | FUSED TRICYCLIC COMPOUNDS AS NOVEL mTOR INHIBITORS - The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R | 2012-07-12 |
20120178745 | Novel Crystalline Oxazine Derivative - The invention relates to 5-cyano-3-methyl-pyridine-2-carboxylic acid [3-((3R,6R)-5-amino-3,6-dimethyl-6-trifluoromethyl-3,6-dihydro-2H-[1,4]oxazin-3-yl)-4-fluoro-phenyl]-amide in crystalline form, to its preparation, its medical use and to medicaments comprising said compound in crystalline form. | 2012-07-12 |
20120178746 | CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula Ik, Im | 2012-07-12 |
20120178747 | Compositions and methods for bone formation and remodeling - The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm. Together with the observation that osteoblast cells produce autocrine canonical Wnt, Wnt7b, and that osteocytes produce paracrine Dkk1, we believe that the G171V mutation may cause an increase in Wnt activity in osteoblasts by reducing the number of targets for paracrine Dkk1 to antagonize without affecting the activity of autocrine Wnt. | 2012-07-12 |
20120178748 | HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes. | 2012-07-12 |
20120178749 | NS1 PROTEIN INHIBITORS - The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention. | 2012-07-12 |
20120178750 | Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I: | 2012-07-12 |
20120178751 | 2-ARYLIMIDAZO[1,2-B]PYRIDAZINE, 2-PHENYLIMIDAZO[1,2-A]PYRIDINE, AND 2-PHENYLIMIDAZO[1,2-A]PYRAZINE DERIVATIVES - Disclosed are compounds of formula (I): | 2012-07-12 |
20120178752 | RHO KINASE INHIBITORS - The present invention relates to compounds of formula (I): | 2012-07-12 |
20120178753 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase. | 2012-07-12 |
20120178754 | Furazano '3, 4-B! Pyrazines and Their Use as Anti-Tumor Agents - The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas. | 2012-07-12 |
20120178755 | CYANOISOQUINOLINE COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure: | 2012-07-12 |
20120178756 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 2012-07-12 |
20120178757 | Method For The Prevention Of Cancer Metastasis - A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient. | 2012-07-12 |
20120178758 | STYRYL-TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS - The invention provides Styryl-Triazine derivatives, and further provides methods of using these compounds to modulate protein kinases and to treat protein kinase mediated diseases. | 2012-07-12 |
20120178759 | CONDENSED PYRIDINE DERIVATIVES USEFUL AS POTENT INHIBITORS OF THE PROTEIN KINASE CK2 - The invention relates to the use of specific compounds of formula (I) and their pharmaceutically-acceptable salts: (Formula 1) (I) as a new family of protein kinase CK2 inhibitors; the invention also relates to the use of compounds of formula (I) for the preparation of pharmaceutical compositions for the prevention and/or treatment of disorders and/or diseases chosen Camongst cancers; autoimmune and inflammatory diseases; infectious diseases; diabetes angiogenesis related disorders; retinopathies and cardiac hypertrophy. | 2012-07-12 |
20120178760 | Heterocyclic-Fused Pyrazolo[4,3-c] Pyridin-3-One M1 Receptor Positive Allosteric Modulators - The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 2012-07-12 |
20120178761 | PYRROLIDINE DERIVATIVES - The invention provides compounds of formula | 2012-07-12 |
20120178762 | COMPOSITIONS OF AZIMILIDE DIHYDROCHLORIDE - The present invention is directed to solvates and various polymorphic forms of (E)-1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione dihydrochloride and pharmaceutical compositions thereof. | 2012-07-12 |
20120178763 | Method of Treating Anxious Major Depressive Disorder - The invention is directed to using 4-{(3-aminophenyl)[4-(4-fluorobenzyl)piperazin-1-yl]methyl}-N,N-diethylbenzamide, or enantiomer thereof, or pharmaceutically acceptable salt thereof, and/or mixture thereof to treat anxious major depressive disorder (AMDD). | 2012-07-12 |
20120178764 | Novel Compounds - The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. | 2012-07-12 |
20120178765 | NOVEL GLUCOKINASE ACTIVATORS AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides an amide derivative having a stilbene or 1,2-diphenylethane moiety within the molecule thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The amide derivative of the present invention activates glucokinase remarkably, and therefore they can be usefully applied for treating glucokinase-mediated diseases, such as hyperglycemia and diabetes. | 2012-07-12 |
20120178766 | FUROPYRIMIDINEDIONE DERIVATIVES AS TRPAI MODULATORS - The present invention is related to novel furopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. | 2012-07-12 |
20120178767 | TREATMENT OF LIVER DISORDERS WITH P13K INHIBITORS - The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments. | 2012-07-12 |
20120178768 | PHOSPHODIESTERASE INHIBITOR TREATMENT - Methods and compositions are disclosed for the treatment of diseases or conditions produced by or associated with low cyclic nucleotide levels. The compositions comprise phosphodiesterase inhibitors and are formulated for intranasal and pulmonary administration. | 2012-07-12 |
20120178769 | NOVEL COMPOUNDS FOR INHIBITING EEF-2 KINASE ACTIVITY - The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof. | 2012-07-12 |
20120178770 | SUBSTITUTED PYRIMIDINYLPYRROLOPYRIDINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS - Pyrimidinylpyrrolopyridinone derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 2012-07-12 |
20120178771 | Oral Pharmaceutical Compositions of Buprenorphine and Method of Use - The present invention is directed to oral, therapeutically effective pharmaceutical compositions of buprenorphine and it pharmaceutically acceptable salts and the use thereof, including delayed onset and controlled release dosage forms. The present invention is also directed delayed onset, rapid release dosage forms and delayed onset, extended release dosage forms of oral buprenorphine which provide robust efficacy and reduced potential for abuse and misuse. | 2012-07-12 |
20120178772 | Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug - The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug. | 2012-07-12 |
20120178773 | Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug - The embodiments provide Compound KC-7, N-1-[(S)-2-(oxycodone-6-enol-carbonyl-methyl-amino)-2-carbonyl-sarcosine-ethyl amine]-arginine-glycine-acetate, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the \compositions comprise a prodrug, Compound KC-7, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug. | 2012-07-12 |
20120178774 | TOLL-LIKE RECEPTOR MODULATORS AND USES THEREOF - The present invention provides a compound selected from the group consisting of: | 2012-07-12 |
20120178775 | METHODS FOR TREATING FRONTOTEMPORAL LOBAR DEGENERATION WITH UBIQUITINATED INCLUSIONS (FTLD-U) - Methods for rescuing learning, memory and/or motor function deficits associated with frontotemporal lobar degeneration with ubiquitinated inclusions (FTLD-U) are disclosed. The method comprises: a) administering to an animal having FTLD-U a therapeutically effective amount of an autophagy inducer; b) causing a decrease in the amount of ubiquitinated TDP-43 aggregation forms in the brain of the animal; and c) causing an improvement of the learning, memory capacities and/or motor function of the animal. | 2012-07-12 |
20120178776 | DIHYDRONAPHTHYRIDINYL(ORGANO)METHANONE ANALOGS AS POSITIVE ALLOSTERIC MGLUR5 MODULATORS - In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2012-07-12 |
20120178777 | Medicaments for Inhibiting Thrombus Formation - A Medicaments for inhibiting thrombus formation contains active ingredients which are triflusal and clopidogrel bisulfate, wherein a mass ratio of triflusal to clopidogrel bisulfate is (100-650):(30-150), preferably (1-20):1, more preferably (3-6):1, and even more preferably 3:1 or 6:1. | 2012-07-12 |
20120178778 | PYRAZOLOPYRIDINES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 2012-07-12 |